Microwave-assisted synthesis of potent PDE7 inhibitors containing a thienopyrimidin-4-amine scaffold.

A series of novel thienopyrimidin-4-amines have been synthesized and evaluated as phosphodiesterase (PDE) inhibitors. A rationale for the observed selectivity against PDE7 has been obtained from molecular modelling studies on the most active compounds.

The diversification of terpene emissions in Mediterranean oaks: lessons from a study of Quercus suber, Quercus canariensis and its hybrid Quercus afares.

Interspecific gene flow is common in oaks. In the Mediterranean, this process produced geographical differentiations and new species, which may have contributed to the diversification of the production of volatile terpenes in the oak species of this region. The endemic North African deciduous oak Quercus afares (Pomel) is considered to be a stabilized hybrid between the evergreen Quercus suber (L.) and the deciduous Quercus canariensis (Willd.), presumably being monoterpene and isoprene emitters, respectively. In a common garden experiment, we examined the terpene emission capacities, terpene synthase (TPS) activities and nuclear genetic markers in 52 trees of these three oak species. All but one of the Q. suber and Q. canariensis trees were found to be genetically pure, whereas most Q. afares trees possessed a mixed genotype with a predominance of Q. suber alleles. Analysis of the foliar terpene emissions and TPS activities revealed that all the Q. canariensis trees strongly produced isoprene while all the Q. suber trees were strong monoterpene producers. Quercus afares trees produced monoterpenes as well but at more variable and significantly lower rates, and with a monoterpene pattern different than that observed in Q. suber. Among 17 individuals tested, one Q. afares tree emitted only an insignificant amount of terpenes. No mixed isoprene/monoterpene emitter was detected. Our results suggest that the capacity and pattern of volatile terpene production in Algerian Q. afares populations have strongly diverged from those of its parental species and became quantitatively and qualitatively reduced, including the complete suppression of isoprene production.

Root anoxia effects on physiology and emissions of volatile organic compounds (VOC) under short- and long-term inundation of trees from Amazonian floodplains.

Volatile organic compound (VOC) emissions are affected by a variety of biotic and abiotic factors such as light intensity, temperature, CO2 and drought. Another stress factor, usually overlooked but very important for the Amazon region, is flooding. We studied the exchange of VOCs in relation to CO2 exchange and transpiration of 8 common tree species from the Amazonian floodplain forest grown up from seeds using a dynamic enclosure system. Analysis of volatile organics was performed by PTR-MS fast online measurements. Our study confirmed emissions of ethanol and acetaldehyde at the beginning of root anoxia after inundation, especially in less anoxia adapted species such as Vatairea guianensis, but not for Hevea spruceana probably due to a better adapted metabolism. In contrast to short-term inundation, long-term flooding of the root system did not result in any emission of ethanol or/and acetaldehyde. Emission of other VOCs, such as isoprenoids, acetone, and methanol exhibited distinct behavior related to the origin (igapó or várzea type of floodplain) of the tree species. Also physiological activities exhibited different response patterns for trees from igapó or várzea. In general, isoprenoid emissions increased within the course of some days of short-term flooding. After a long period of waterlogging, VOC emissions decreased considerably, along with photosynthesis, transpiration and stomatal conductance. However, even under long-term testing conditions, two tree species did not show any significant decrease or increase in photosynthesis. In order to understand ecophysiological advantages of the different responses we need field investigations with adult tree species.

Male eating disorders and therapy: a controlled pilot study with one year follow-up.

OBJECTIVES: To examine whether outpatient treatment for male patients with bulimic symptomatology is as effective as it is for females. METHOD: The outcome of 19 male patients was compared to that of 150 female eating disorder (ED) individuals after a group CBT treatment. RESULTS: A reduction in ED symptomatology was observed after treatment for both genders. Main effects for gender indicated that after collapsing across the mean pre/post values, lower mean scores were found for men in the EAT-40, in the EDI-total score and in the following EDI subscales: "drive for thinness", "body dissatisfaction" and "interoceptive awareness". CONCLUSIONS: A group CBT treatment appears to be effective for male and female ED patients.

Internet-based cognitive-behavioral therapy for bulimia nervosa: a controlled study.

The object of this study was to examine the effectiveness of an Internet-based therapy (IBT) for bulimia nervosa (BN) as compared to a waiting list (WL). Sixty-two female BN patients, diagnosed according to DSM-IV criteria, were assigned to either the IBT or a WL. The control participants (WL) were matched to the IBT group in terms of age, duration of the disorder, number of previous treatments, and severity of the disorder. Assessment measures included the EDI, SCL-90-R, BITE, the TCI-R, and other clinical and psychopathological indices, which were administrated before and after the treatment. Considering the IBT, while the mean scores were lower at the end of the treatment for some EDI scales (bulimic, interpersonal distrust, maturity fears, and total score) and the BITE symptomatology subscale, the mean BMI was higher at posttherapy. Predictors of good IBT outcome were higher scores on the EDI perfectionism scale and EAT and a higher minimum BMI. Drop-out (after IBT 35.5% of cases) was related to higher SCL-anxiety scores, a lower hyperactivity, a lower minimum BMI, and lower TCI-reward dependence scores. At the end of the treatment, bingeing and vomiting abstinence rates differed significantly between the two groups. Results suggest that an online self-help approach appears to be a valid treatment option for BN when compared to a WL control group, especially for people who present a lower severity of their eating disorder (ED) symptomatology and some specific personality traits.

A new class of pyrazolopyridine nucleus with fluorescent properties, obtained through either a radical or a Pd arylation pathway from N-azinylpyridinium N-aminides.

The synthesis of dipyridopyrazole and pyridopyrazolopyrazine derivatives--both of which incorporate a 3-aryl moiety--can be achieved in moderate yields by intramolecular radical arylation of pyridinium N-aminides using tris(trimethylsilyl)silane and azobisisobutyronitrile. Improved results were obtained on using Pd direct arylation in conjunction with microwave irradiation. A preliminary study into the fluorescent properties of the target compounds is also reported.

Contribution of the serotoninergic system to anxious and depressive traits that may be partially responsible for the phenotypical variability of bulimia nervosa.

Eating disorders (ED), such as anorexia nervosa (AN) and bulimia nervosa (BN), are complex psychiatric phenotypes influenced by both genetic and environmental factors. We investigated the genetic contribution of four single nucleotide polymorphisms (SNPs) within the serotonin receptor 5HT2C and two sequence variants within the serotonin transporter SLC6A4 to different ED-related psychopathological symptoms in a total sample of 82 ED patients. All patients were diagnosed according to DSM-IV criteria and underwent diagnostic and psychopathological assessments by means of structured clinical interviews and rating scales. We detected significant evidence of association between the -995A/-759T/-697C/Cys23 haplotype of the 5HT2C gene and different anxious and depressive subscales of the SCL90-R instrument, that included Somatization (p = 0.029), Obsessive-Compulsiveness (p = 0.021), Depression (p = 0.032), Anxiety (p = 0.004), Hostility (p = 0.028), Phobic Anxiety (p = 0.029) and Paranoid Ideation (p = 0.008), in BN patients. We also observed a strong association between the 5HTTLPR polymorphism of the SLC6A4 gene and Anxiety in the same group of BN patients (p = 0.004). However, no epistatic effects between the 5HT2C and SLC6A4 genes on the different anxious and depressive subscales were observed. Our preliminary data suggest that the serotoninergic system contributes to the different psychopathological symptoms that may be partially responsible for the phenotypical variability within the bulimic phenotype.

Eficacia del tratamiento ambulatorio cognitivo-conductual en la bulimia nerviosa / No disponible

El objetivo del presente estudio fue analizar la eficacia de dos tipos de terapias grupales (TG) (psicoeducativa –PE- vs. cognitivo-conductual –CBT-) en bulimia nervosa (BN), al ser comparados los datos con un grupo de control en lista de espera. Participaron en el presente estudio 100 pacientes con BN, diagnosticados según criterios del DSM-IV, que acudieron de forma consecutiva a tratamiento a nuestra Unidad de trastornos alimentarios. La muestra total fue asignada de forma consecutiva: (a) TG de corta duración (PE, N=50) (b) TG larga duración (CBT, N=50). Los datos fueron comparados con un grupo de control (GC), formado por 40 pacientes con BN, emparejados por edad por edad, gravedad y duración del trastorno, que se encontraban en lista de espera. Todos los pacientes eran del sexo femenino. Fueron utilizados cuestionarios aplicados comúnmente en este ámbito de investigación, tales como Eating Disorders Inventory (EDI), Bulimic Investigatory Test Edinburgh (BITE), Eating Attitudes Test (EAT-40), Social Avoidance Scale (SAD), Body Shape Questionnaire (BSQ) y Beck Depression Inventory (BDI). Como medidas de recuperación fueron también utilizadas la frecuencia semanal de atracones y vómitos. Tras el tratamiento, el grado de abstinencia de atracones varió significativamente entre los grupos (X2=37,13; p< 0,001), oscilando entre 72% en CBT, 33% en PE y 8% GC. El grado de eficacia a corto-plazo, 75,6% en CBT vs. 38,1% en PE, mostró ir asociado a la variable independiente (PE vs. CBT- p< 0,001), mientras que el no-tratamiento (GC) tuvo como consecuencia un aumento en el IMC de los pacientes (t-pairs= -2,38, p< 0,024). Como factores predictores de eficacia de tratamiento fueron encontrados los siguientes: menor gravedad del trastorno (p< 0,018) y un más tardío inicio del TCA (p< 0,05). Como conclusión principal del estudio, destacaríamos que CBT (TG larga) muestra mejores resultados que PE (TG corta), mientras que el no-tratamiento no mostraría remisión espontánea. PE estará especialmente indicada en pacientes con menor gravedad del trastorno (AU)

No disponible